The detection of protamine is meaningful however, the detection of protamine is difficult due to the lack of aromatic amino acids in its composition. The mechanisms involve membrane receptors and ion channels targeted by different vasoactive compounds, such as nitric oxide, bradykinin or histamine. Protamine, an arginine-rich polycationic peptide, is a natural food preservative and the only approved antidote to heparin overdose. 4 Despite the frequent use of LMWH, there are few descriptions of management strategies for LMWH overdoses. This effect may be largely neutralized by slow intravenous injection of protamine sulfate. Protamine sulphate is composed of polypeptides that bind heparin to form a stable, inactive complex that inhibits the antifactor IIa effect of LMWH, 1 but the effect on antifactor Xa is only partial, 2, 3 reaching up to 74. The cationic hydrogenated protamine at a pH of 6.8 to 7.1 reacts with anionic heparin at a pH of 5.0 to 7.5 to form an inactive complex. CONTRAINDICATIONS: Protamine sulfate is contraindicated in patients who have shown previous intolerance to the drug. The toxicology of protamine depends on a complex interaction of the high molecular weight, a cationic peptide with the surfaces of the vasculature and blood cells. The anticoagulant effect of LOVENOX is inhibited by protamine. INDICATIONS AND USAGE: Protamine Sulfate Injection, USP is indicated in the treatment of heparin overdosage. In accidental overdoses of heparin, consider t1/2 heparin 60-90 min. Monitor APTT 5-15 min after dose then in 2-8 hr. Past and present knowledge of the mechanisms responsible for the toxicity of protamine and the most promising potential replacements of protamine in the different phases of development.ĭespite of the low therapeutic index, protamine is the only registered antidote of heparins. Background: Protamine sulfate is the antidote for heparin, but in excess it exerts weak anticoagulation. 1-1.5 mg per 100 USP units of heparin not to exceed 50 mg. In addition, the clinically applied antidote for heparin, protamine, is a histone-like DNA-binding protein which replaces histones in spermatogenesis to allow for DNA condensation 11. Recent studies have demonstrated new organ-specific complications of the heparin reversal with protamine. Despite its extensive clinical use, protamine may produce life-threatening side effects such as systemic hypotension, catastrophic pulmonary vasoconstriction or allergic reactions. In the case of an emergency bleeding in response to heparin, the protamine sulfate is administered. Bleeding resulting from the application of low-molecular-weight heparins (LMWHs) may be treated with protamine sulfate, but this treatment lacks efficiency its. Unfractionated heparin is a strongly anionic anticoagulant used extensively in medicine to prevent blood clotting.
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